Jiangsu Key Laboratory of Drug Design & Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, PR China.
Jiangsu Key Laboratory of Drug Design & Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, PR China.
Eur J Med Chem. 2020 Oct 1;203:112539. doi: 10.1016/j.ejmech.2020.112539. Epub 2020 Jul 15.
Proteolysis-targeting chimeric molecules (PROTACs), which attract much more attention today, may be a potential way to treat cancer. PROTACs are made up of ligands of target proteins, E3 ligase recruiting elements and linkers. PROTACs can hijack the intracellular inherent ubiquitin proteasome system in cells to degrade different target proteins. PROTACs targeting different cancer-related proteins have been successfully developed and outperform small inhibitors, the traditional way of treating cancer. In this review, we focus on PROTACs targeting cancer-related proteins and their superiority over inhibitors.
蛋白水解靶向嵌合体（PROTACs），如今受到了更多的关注，可能是治疗癌症的一种潜在方法。PROTACs 由靶蛋白的配体、E3 连接酶募集元件和连接子组成。PROTACs 可以劫持细胞内固有的泛素蛋白酶体系统来降解不同的靶蛋白。针对不同的癌症相关蛋白的 PROTACs 已经被成功开发出来，并优于传统的治疗癌症的小分子抑制剂。在这篇综述中，我们重点介绍了针对癌症相关蛋白的 PROTACs 及其优于抑制剂的优势。
